| 产品描述: | Lexibulin (CYT-997) is a potent and orally active tubulin polymerisation inhibitor with IC50s of 10-100 nM in cancer cell lines; with potent cytotoxic and vascular disrupting activity in vitro and in vivo. Lexibulin induces cell apoptosis and induces mitochondrial ROS generation in GC cells |
| 靶点: |
IC50 value: 10-100 nM(cell assay);Apoptosis; ReactiveOxygenSpecies; MicrotubuleAssociated |
| 体内研究: |
iIn a xenograft model using the human prostate cancer cell line PC3, oral dosing of Lexibulin (CYT-997) is initiated 13 days after cell implantation by which time palpable tumors were evident. A dose-dependent inhibition of tumor growth was apparent with Lexibulin (CYT-997), which at the highest dose was equivalent to parenterally administered paclitaxel. A single dose of Lexibulin (CYT-997) (7.5 mg/kg i.p.) clearly decreased blood flow in liver metastases, and a significant reduction in blood flow was present 6 hours postdose. Lexibulin (CYT-997) treatment (15 mg/kg/day) significantly prolongs the survival in a murine model of aggressive systemic myelomatosis |
| 参考文献: |
1. Burns CJ, et al. CYT997: a novel orally active tubulin polymerization inhibitor with potent cytotoxic and vascular disrupting activity in vitro and in vivo. Mol Cancer Ther. 2009 Nov;8(11):3036-45. 2. Monaghan K, et al. CYT997 causes apoptosis in human multiple myeloma. Invest New Drugs. 2011 Apr;29(2):232-8. 3. Ya Cao, wt al. Mitochondrial ROS Accumulation Inhibiting JAK2/STAT3 Pathway Is a Critical Modulator of CYT997-induced Autophagy and Apoptosis in Gastric Cancer. J Exp Clin Cancer Res. 2020 Jun 23;39(1):119. |
| 溶解性: |
DMSO : ≥ 100 mg/mL (230.13 mM) |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.301 ml |
11.507 ml |
23.013 ml |
| 5 mM |
0.46 ml |
2.301 ml |
4.603 ml |
| 10 mM |
0.23 ml |
1.151 ml |
2.301 ml |
| 50 mM |
0.046 ml |
0.23 ml |
0.46 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |